CA2506290C - 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases - Google Patents

17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases Download PDF

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Publication number
CA2506290C
CA2506290C CA2506290A CA2506290A CA2506290C CA 2506290 C CA2506290 C CA 2506290C CA 2506290 A CA2506290 A CA 2506290A CA 2506290 A CA2506290 A CA 2506290A CA 2506290 C CA2506290 C CA 2506290C
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CA
Canada
Prior art keywords
compound
isomer
pharmaceutically acceptable
solvate
acceptable salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2506290A
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English (en)
French (fr)
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CA2506290A1 (en
Inventor
Kamil Paruch
Timothy J. Guzi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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Publication of CA2506290A1 publication Critical patent/CA2506290A1/en
Application granted granted Critical
Publication of CA2506290C publication Critical patent/CA2506290C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/12Keratolytics, e.g. wart or anti-corn preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2506290A 2002-11-18 2003-11-14 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases Expired - Fee Related CA2506290C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42726302P 2002-11-18 2002-11-18
US60/427,263 2002-11-18
PCT/US2003/036203 WO2004046111A1 (en) 2002-11-18 2003-11-14 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases

Publications (2)

Publication Number Publication Date
CA2506290A1 CA2506290A1 (en) 2004-06-03
CA2506290C true CA2506290C (en) 2012-04-24

Family

ID=32326512

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2506290A Expired - Fee Related CA2506290C (en) 2002-11-18 2003-11-14 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases

Country Status (16)

Country Link
US (2) US7074795B2 (https=)
EP (1) EP1562901B1 (https=)
JP (2) JP4614770B2 (https=)
CN (1) CN100374421C (https=)
AR (1) AR042046A1 (https=)
AT (1) ATE469886T1 (https=)
AU (1) AU2003290799A1 (https=)
CA (1) CA2506290C (https=)
CL (1) CL2003002356A1 (https=)
DE (1) DE60332862D1 (https=)
ES (1) ES2345146T3 (https=)
MX (1) MXPA05005360A (https=)
MY (1) MY130792A (https=)
PE (1) PE20040750A1 (https=)
TW (1) TW200412964A (https=)
WO (1) WO2004046111A1 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60323765D1 (de) 2002-12-17 2008-11-06 Schering Corp Inhibitoren der 17 beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
US7851474B2 (en) * 2005-08-02 2010-12-14 Neurogen Corporation Dipiperazinyl ketones and related analogues
US8080540B2 (en) 2006-09-19 2011-12-20 Abbott Products Gmbh Therapeutically active triazoles and their use
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
US8501940B2 (en) * 2008-07-15 2013-08-06 Hoffmann-La Roche Inc. Tetrahydrocinnoline derivatives
CN106890100A (zh) * 2011-04-25 2017-06-27 朴俊炯 用于预防脱发和促进毛发生长的局部施用的组合物
TW201512215A (zh) 2013-06-25 2015-04-01 Forendo Pharma Ltd 治療活性雌三烯噻唑衍生物
JP6556125B2 (ja) 2013-06-25 2019-08-07 フォレンド ファーマ リミテッド 17β−ヒドロキシステロイドデヒドロゲナーゼの阻害剤としての治療的に活性な17−窒素置換エストラトリエンチアゾール誘導体
JP6456373B2 (ja) 2013-06-25 2019-01-23 フォレンド ファーマ リミテッド 17β−ヒドロキシステロイドデヒドロゲナーゼ タイプ1の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体
JP6545266B2 (ja) 2014-12-23 2019-07-17 フォレンド ファーマ リミテッド 17β‐HSD1抑制剤のプロドラッグ
CN107207561B (zh) 2014-12-23 2020-03-31 佛恩多制药有限公司 17β-HSD1–抑制剂的前药
JP6532599B2 (ja) 2015-09-02 2019-06-19 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド
HRP20240679T1 (hr) 2017-06-08 2024-08-16 Organon R&D Finland Ltd 17-oksimi 15.beta.-[3-propanamido]-supstituiranih etera-1,3,5(10)-trien-17-ona za uporabu u inhibiciji 17.beta.-hidroksisteroid dehidrogenaza
AU2018386327B2 (en) * 2017-12-15 2023-04-13 Inthera Bioscience AG 1 -(piperidinocarbonylmethyl)-2-oxopiperazine derivatives for treating cancer
JP7417608B2 (ja) 2018-12-05 2024-01-18 フォレンド ファーマ リミテッド 17-hsd1阻害剤としての16(17)位でピラゾール環と縮合しているエストラ-1,3,5(10)-トリエン化合物
EP4168014A1 (en) 2020-06-19 2023-04-26 Inthera Bioscience AG Oxopiperazine derivatives for the treatment of cancer

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE58836B1 (en) 1984-08-02 1993-11-17 Labrie Fernand Pharmaceutical composition for combination therapy of hormone dependent cancers
ZA901847B (en) 1989-03-10 1991-10-30 Endorecherche Inc Combination therapy for the treatment of estrogen sensitive diseases
ATE230994T1 (de) 1989-07-07 2003-02-15 Endorech Inc Methode zur behandlung androgenbedingter krankheiten
DE69034148T2 (de) 1989-07-07 2005-06-30 Endorecherche Inc., Ste-Foy Kombinationstherapie zur Prophylaxe und/oder Behandlung von gutartiger prostatischer Hyperplasie
US6060503A (en) 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
ATE197458T1 (de) 1993-05-17 2000-11-11 Endorech Inc Verbesserte antiandrogene
US6124115A (en) 1995-09-22 2000-09-26 Endorecherche Inc. Production and use of isolated type 5 17β-hydroxysteroid dehydrogenase
AU4801197A (en) * 1996-09-13 1998-04-02 Schering Corporation Tricyclic antitumor compounds being farnesyl protein transferase inhibit ors
HUP0101809A3 (en) * 1998-03-11 2002-07-29 Endorech Inc Sainte Foy Inhibitors of type 5 and type 3 17betha-hydroxysteroid dehydrogenase and methods for their use
PE20030703A1 (es) 2001-09-06 2003-08-21 Schering Corp Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3
EP1436281B1 (en) * 2001-10-17 2010-06-16 Schering Corporation Piperidine- and piperazineacetamides as 17beta hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases

Also Published As

Publication number Publication date
CA2506290A1 (en) 2004-06-03
CN1738800A (zh) 2006-02-22
AR042046A1 (es) 2005-06-08
CN100374421C (zh) 2008-03-12
JP2010138204A (ja) 2010-06-24
US7476681B2 (en) 2009-01-13
MY130792A (en) 2007-07-31
AU2003290799A1 (en) 2004-06-15
US20040127503A1 (en) 2004-07-01
WO2004046111A1 (en) 2004-06-03
US7074795B2 (en) 2006-07-11
ATE469886T1 (de) 2010-06-15
CL2003002356A1 (es) 2005-02-11
TW200412964A (en) 2004-08-01
EP1562901B1 (en) 2010-06-02
DE60332862D1 (de) 2010-07-15
US20060148816A1 (en) 2006-07-06
PE20040750A1 (es) 2004-11-06
JP2006513169A (ja) 2006-04-20
JP4614770B2 (ja) 2011-01-19
HK1073313A1 (en) 2005-09-30
EP1562901A1 (en) 2005-08-17
ES2345146T3 (es) 2010-09-16
MXPA05005360A (es) 2005-08-03

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Effective date: 20141114